Related Experiment Videos
Substituted indole-5-carboxamides and -acetamides as potent nonpeptide GnRH receptor antagonists
W T Ashton1, R M Sisco, Y T Yang
1Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, 07065-0900, Rahway, NJ, USA. wally_ashton@merck.com
Bioorganic & Medicinal Chemistry Letters
|June 27, 2001
Abstract:
The 2-aryltryptamine class of GnRH receptor antagonists has been modified to incorporate carboxamide and acetamide substituents at the indole 5-position. With either a phenol or methanesulfonamide terminus on the N-aralkyl side chain, potent binding affinity to the GnRH receptor was achieved. A functional assay for GnRH antagonism was even more sensitive to structural modification and revealed a strong preference for branched tertiary amides.